A Study to Evaluate How Well Single and Multiple Doses of GLPG3121-modified Release Formulation Are Tolerated in Healthy, Adult Subjects

• ClinicalTrials.gov Identifier: NCT04856358
• Recruitment Status: Completed
• First Posted: April 23, 2021
• Last Update Posted: December 3, 2021
• Sponsor: Galapagos NV
• Information provided by (Responsible Party): Galapagos NV

Study Description

Brief Summary:

The aim of the study is to examine the safety and tolerability of GLPG3121-modified release formulation when given to healthy male subjects once as a single dose or multiple times over a period of 14 days in fasting condition or after a standard breakfast.

The study will evaluate how the body absorbs and breaks down GLPG3121, and how GLPG3121 and the major breakdown product of GLPG3121 are eliminated from the body. In addition, the study will investigate the effect of food (high-fat) after a single oral dose of GLPG3121 as modified release tablet.

Condition or disease	Intervention/treatment	Phase
Healthy	Drug: GLPG3121; Drug: Placebo	Phase 1

Study Design

• Study Type: Interventional (Clinical Trial)
• Actual Enrollment: 50 participants
• Allocation: Randomized
• Intervention Model: Parallel Assignment
• Intervention Model Description: Part 1 Single Ascending Dose (SAD) and Part 2 Multiple Ascending Dose (MAD) are randomized, double-blind, placebo-controlled; Part 3 Food-effect (FE) is randomized, open-label, crossover
• Masking: Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)
• Primary Purpose: Basic Science
• Official Title: A Phase I, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single and Multiple Ascending Oral Doses of GLPG3121-modified Release Formulation in Adult, Healthy, Male Subjects
• Actual Study Start Date: April 27, 2021
• Actual Primary Completion Date: November 8, 2021
• Actual Study Completion Date: November 8, 2021

Arms and Interventions

Arm	Intervention/treatment
Experimental: GLPG3121 SAD; Single doses of GLPG3121 at up to 3 dose levels in ascending order	Drug: GLPG3121; GLPG3121 modified-release tablet
Placebo Comparator: Placebo SAD; Single doses of placebo	Drug: Placebo; Matching placebo
Experimental: GLPG3121 MAD; Multiple doses of GLPG3121 at up to 3 dose levels in ascending order	Drug: GLPG3121; GLPG3121 modified-release tablet
Placebo Comparator: Placebo MAD; Multiple doses of placebo	Drug: Placebo; Matching placebo
Experimental: GLPG3121 FE fed; Single dose of GLPG3121 in fed state	Drug: GLPG3121; GLPG3121 modified-release tablet
Experimental: GLPG3121 FE fasted; Single dose of GLPG3121 in fasted state	Drug: GLPG3121; GLPG3121 modified-release tablet

Outcome Measures

Primary Outcome Measures :

1. Frequency and severity of treatment emergent adverse events (TEAEs), treatment-emergent serious adverse events, and TEAEs leading to treatment discontinuations [ Time Frame: From screening through study completion, an average of 8 months ]
   To evaluate the safety and tolerability of single and multiple ascending oral doses of GLPG3121-modified-release formulation (GLPG3121-MR), in adult, healthy, male subjects compared with placebo

Secondary Outcome Measures :

1. Maximum observed plasma concentration (Cmax) of GLPG3121 in SAD [ Time Frame: Between Day 1 pre-dose and Day 6 ]
   To evaluate the pharmacokinetics (PK) of single ascending oral doses of GLPG3121 in adult, healthy, male subjects
2. Cmax of GLPG3121's main metabolite in SAD [ Time Frame: Between Day 1 pre-dose and Day 6 ]
   To evaluate the PK of single ascending oral doses of GLPG3121's metabolite in adult, healthy, male subjects
3. Cmax of GLPG3121 in MAD [ Time Frame: Between Day 1 pre-dose and Day 19 ]
   To evaluate the PK of multiple ascending oral doses of GLPG3121 in adult, healthy, male subjects
4. Cmax of GLPG3121's main metabolite in MAD [ Time Frame: Between Day 1 pre-dose and Day 19 ]
   To evaluate the PK of multiple ascending oral doses of GLPG3121's main metabolite in adult, healthy, male subjects
5. Area under the plasma concentration-time curve (AUC) of GLPG3121 in SAD [ Time Frame: Between Day 1 pre-dose and Day 6 ]
   To evaluate the PK of single ascending oral doses of GLPG3121 in adult, healthy, male subjects
6. AUC of GLPG3121's main metabolite in SAD [ Time Frame: Between Day 1 pre-dose and Day 6 ]
   To evaluate the PK of single ascending oral doses of GLPG3121's main metabolite in adult, healthy, male subjects
7. AUC of GLPG3121 in MAD [ Time Frame: Between Day 1 pre-dose and Day 19 ]
   To evaluate the PK of multiple ascending oral doses of GLPG3121 metabolite in adult, healthy, male subjects
8. AUC of GLPG3121's main metabolite in MAD [ Time Frame: Between Day 1 pre-dose and Day 19 ]
   To evaluate the PK of multiple ascending oral doses of GLPG3121's main metabolite in adult, healthy, male subjects
9. Terminal elimination half-life (t1/2) of GLPG3121 in SAD [ Time Frame: Between Day 1 pre-dose and Day 6 ]
   To evaluate the PK of single ascending oral doses of GLPG3121 in adult, healthy, male subjects
10. t1/2 of GLPG3121's main metabolite in SAD [ Time Frame: Between Day 1 pre-dose and Day 6 ]
    To evaluate the PK of single ascending oral doses of GLPG3121's main metabolite in adult, healthy, male subjects
11. t1/2 of GLPG3121 in MAD [ Time Frame: Between Day 1 pre-dose and Day 19 ]
    To evaluate the PK of multiple ascending oral doses of GLPG3121 in adult, healthy, male subjects
12. t1/2 of GLPG3121's main metabolite in MAD [ Time Frame: Between Day 1 pre-dose and Day 19 ]
    To evaluate the PK of multiple ascending oral doses of GLPG3121's main metabolite in adult, healthy, male subjects

Eligibility Criteria

• Ages Eligible for Study: 18 Years to 55 Years (Adult)
• Sexes Eligible for Study: Male
• Accepts Healthy Volunteers: Yes

Criteria

Inclusion Criteria:

• Male between 18 and 55 years of age (extremes included), on the date of signing the informed consent form (ICF).
• A body mass index (BMI) between 18.0 and 30.0 kg/m2, inclusive.
• Judged to be in good health by the investigator based upon the results of a medical history, physical examination, vital signs, 12-lead electrocardiogram (ECG), and fasting clinical laboratory safety tests, available at screening and prior to randomization. Hemoglobin, neutrophil, lymphocyte, and platelet counts must be above the lower limit of normal range. Total bilirubin, aspartate aminotransferase (AST), alanine aminotransferase (ALT), and serum creatinine must be no greater than the upper limit of normal (ULN). Other clinical laboratory safety test results must be within the reference ranges or test results that are outside the reference ranges need to be considered not clinically significant in the opinion of the investigator.
• Subject must be able and willing to comply with restrictions on prior and concomitant medication.
• Negative screen for drugs (amphetamines, barbiturates, benzodiazepines, cannabis, cocaine, opiates, methadone, tricyclic antidepressants) and alcohol.

This list only contains the key inclusion criteria.

Exclusion Criteria:

• Known hypersensitivity to investigational product (IP) ingredients or history of a significant allergic reaction to IP ingredients as determined by the investigator.
• Positive serology for hepatitis B virus surface antigen (HBsAg) or hepatitis C virus (HCV) or history of hepatitis from any cause with the exception of hepatitis A that was resolved at least 3 months prior to first dosing of the IP.
• History of or a current immunosuppressive condition (e.g. human immunodeficiency virus [HIV] infection).
• Having any illness, judged by the investigator as clinically significant, in the 3 months prior to first dosing of the IP.
• Presence or sequelae of gastrointestinal, liver, kidney (estimated glomerular filtration rate [eGFR] <=90 mL/min/1.73 m2, using the Chronic Kidney Disease Epidemiology Collaboration [CKD-EPI] formula) or other conditions known to interfere with the absorption, distribution, metabolism, or excretion of drugs.

This list only contains the key exclusion criteria.

Contacts and Locations

Locations

Germany

Charité Research Organisation GmbH

Berlin, Germany, 10117

Sponsors and Collaborators

Galapagos NV

Investigators

• Study Director: Magdalena Petkova, MD; Galapagos NV

More Information

• Responsible Party: Galapagos NV
• ClinicalTrials.gov Identifier: NCT04856358
• Other Study ID Numbers: GLPG3121-CL-103; 2020-004174-21 ( EudraCT Number )
• First Posted: April 23, 2021
• Last Update Posted: December 3, 2021
• Last Verified: December 2021

Individual Participant Data (IPD) Sharing Statement:

• Plan to Share IPD: No

• Studies a U.S. FDA-regulated Drug Product: No
• Studies a U.S. FDA-regulated Device Product: No